Nolvadex: Targeted Estrogen Blockade for Breast Cancer Management
Nolvadex
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Synonyms
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Nolvadex (tamoxifen citrate) is a cornerstone selective estrogen receptor modulator (SERM) used in the hormonal therapy of breast cancer. It represents one of the most extensively studied and clinically validated oral endocrine treatments in oncology. By competitively antagonizing estrogen receptors in breast tissue, Nolvadex disrupts the hormone-dependent proliferation of malignant cells, offering a targeted mechanism of action. Its well-established efficacy profile and generally favorable tolerability have secured its position as a first-line and adjuvant therapeutic option for decades, benefiting both premenopausal and postmenopausal patients with hormone receptor-positive disease.
Features
- Active Pharmaceutical Ingredient: Tamoxifen citrate
- Standard Tablet Strengths: 10 mg and 20 mg
- Pharmacologic Class: Selective Estrogen Receptor Modulator (SERM)
- Administration Route: Oral
- Bioavailability: High, with peak plasma concentrations reached within 4-7 hours post-ingestion
- Half-life: Approximately 5-7 days for the primary active metabolite, endoxifen
- Metabolism: Hepatic, primarily via CYP2D6 and CYP3A4 isoenzymes
Benefits
- Significantly reduces the risk of recurrence in early-stage, hormone receptor-positive breast cancer.
- Lowers the incidence of contralateral breast cancer in high-risk individuals.
- Provides a non-cytotoxic, well-tolerated oral treatment option, supporting patient quality of life.
- Offers a therapeutic strategy for both premenopausal and postmenopausal women.
- Serves as a first-line treatment option for metastatic hormone receptor-positive breast cancer.
- Can be used for ovulation induction in fertility treatment under specialist supervision.
Common use
Nolvadex is primarily indicated for the treatment and risk reduction of breast cancer. Its use is strictly confined to patients with estrogen receptor-positive (ER+) or progesterone receptor-positive (PR+) tumors. In early-stage breast cancer, it is used as adjuvant therapy following primary treatment (surgery, radiation, chemotherapy) to prevent disease recurrence. For advanced or metastatic breast cancer, it is used as a primary hormonal treatment to control disease progression. Additionally, it is approved for the reduction of breast cancer incidence in high-risk women. Off-label, it is sometimes utilized by medical specialists to treat other conditions like gynecomastia or for ovulation induction in certain anovulatory disorders.
Dosage and direction
Dosage is individualized based on the specific indication, disease stage, and patient factors. It must be prescribed by a qualified oncologist or physician.
- Breast Cancer Treatment (Adjuvant & Metastatic): The standard adult dosage is 20 mg once daily. Doses exceeding 20 mg daily should be administered as divided doses (e.g., 20 mg twice daily for a 40 mg total dose).
- Breast Cancer Risk Reduction: The recommended dosage is 20 mg once daily for 5 years.
- Administration: Tablets can be taken with or without food. Adherence to a consistent daily schedule is critical for therapeutic efficacy. If gastrointestinal upset occurs, administration with food may be advised.
Precautions
- Ophthalmic Exams: Regular ophthalmological examinations are recommended due to the risk of retinopathy, corneal opacities, and cataracts.
- Liver Function: Periodic liver function tests should be performed, as hepatic adverse effects including fatty liver, cholestasis, and hepatitis can occur.
- Blood Counts: Regular monitoring of blood counts is advised; leukopenia and thrombocytopenia have been observed.
- Hypercalcemia: Patients with bone metastases may experience a transient increase in bone pain and hypercalcemia within weeks of initiating therapy; close monitoring is required.
- Uterine Changes: Women are advised to promptly report any unusual vaginal bleeding, menstrual irregularities, or pelvic pain/pressure, as these may signal endometrial changes.
Contraindications
Nolvadex is contraindicated in patients with:
- Known hypersensitivity to tamoxifen citrate or any component of the formulation.
- A history of deep vein thrombosis (DVT) or pulmonary embolism (PE).
- Concurrent anticoagulant therapy with warfarin (requires extreme caution and is often a contraindication).
- Women who are pregnant or may become pregnant, as it may cause fetal harm. Pregnancy must be excluded before initiation. Effective non-hormonal contraception is mandatory during and for several months after treatment.
Possible side effect
Common side effects are often related to its anti-estrogenic effects and may include:
- Very Common (>10%): Hot flashes, vaginal discharge or dryness, nausea, fatigue.
- Common (1-10%): Fluid retention, skin rash, pruritus vulvae, vomiting, menstrual irregularities, alopecia, headache, dizziness, depression.
- Serious (require immediate medical attention): Signs of thromboembolism (unilateral leg swelling, chest pain, dyspnea), unusual vaginal bleeding, visual disturbances, signs of liver dysfunction (jaundice, dark urine), severe abdominal pain (pancreatitis), signs of stroke.
Drug interaction
Nolvadex has several clinically significant interactions:
- CYP2D6 Inhibitors (e.g., Paroxetine, Fluoxetine, Quinidine, Bupropion): May significantly reduce the conversion of tamoxifen to its potent active metabolite, endoxifen, potentially diminishing its efficacy. Concomitant use should be avoided if possible.
- Warfarin: Markedly potentiates the anticoagulant effect, increasing the risk of serious or life-threatening bleeding. INR must be monitored very closely if co-administration is unavoidable.
- CYP3A4 Inducers (e.g., Rifampin, Phenytoin, St. John’s Wort): May increase the metabolism of tamoxifen, reducing its plasma concentration and effectiveness.
- Cytotoxic Chemotherapy: May increase the risk of thromboembolic events when used in combination.
Missed dose
If a dose is missed, it should be taken as soon as it is remembered on the same day. If the missed dose is not remembered until the next day, the patient should skip the missed dose and resume the usual dosing schedule. Do not double the dose to make up for a missed one. Maintaining a consistent daily routine is important for efficacy.
Overdose
There is no specific antidote for tamoxifen overdose. Symptoms may be an exaggeration of known side effects, including nausea, vomiting, dizziness, tremor, and headache. Severe overdose may lead to QT prolongation. In cases of acute overdose, supportive and symptomatic treatment is essential. Due to the long half-life, monitoring should be prolonged. Medical attention must be sought immediately.
Storage
Store at room temperature (20°C to 25°C or 68°F to 77°F), in a tightly closed container. Protect from light and moisture. Keep out of reach of children and pets. Do not flush medication down the toilet or pour it into a drain. Dispose of unused medication through a medicine take-back program.
Disclaimer
This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your qualified physician or other licensed healthcare provider with any questions you may have regarding a medical condition or treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here. The content has not been evaluated by all regulatory bodies and is intended for an expert audience.
Reviews
- “As a practicing oncologist for over 25 years, Nolvadex remains a fundamental tool in our arsenal for ER+ breast cancer. Its efficacy in reducing recurrence is robustly proven by decades of clinical trial data. While side effects like hot flashes are common, they are often manageable, and the benefit-risk profile for appropriate patients is overwhelmingly positive.”
- “From a clinical research perspective, the long-term follow-up data from trials like NSABP B-14 and IBIS-I continue to validate the profound impact of 5 years of tamoxifen therapy on long-term survival and risk reduction. The understanding of its metabolite, endoxifen, and the role of CYP2D6 pharmacogenomics has added a layer of precision to its application.”
- “In my pharmacy practice, patient education on adherence and side effect management is key. The long half-life is a double-edged sword; it allows for some forgiveness with timing but also means side effects can persist for some time after discontinuation. The drug interaction profile, particularly with SSRIs, requires vigilant medication review.”